Relationship Between Chemical Structure and Antibacterial Activity in Methylated Isoxazolylnaphthoquinones

PATRICIA BOGDANOV, CRISTINA ORTIZ, ALBERTO ERASO AND INÉS ALBESA

BIRKHAUSER BOSTON INC

Año: 2001 p. 577 - 577

elationship between chemical structure and antibacterial activity of six isoxazolylnaphthoquinones was studied against Staphylococcus aureus including methicillin resistant strain. Two drugs were enolic compounds and the others were their ketonic derivatives and their bis-isozaxolylnaphthoquinone derivatives Bacteria were inhibited by the stimuli of superoxide anion produced by the new drugs. generated more S. aureus than the other compounds. Introduction of a second methyl group in C-3 of the isoxazol ring reduced the antibacterial activity and generation. A second aminoisoxazolyl function in C-2 of the naphthoquinone ring inhibited the biological activity. The log Poct was determined by HPLC to establish its relationship with the antibiotic potency. High correlation was found between log Poct and log k´w